Aqueous compositions

Abstract

Suggested is a non-therapeutic aqueous composition for topical application, comprising (a) at least one solid active agent having at 20° C. a solubility in water (20° dH) of less than 5 g/L; (b) at least one 1,2-alkandiol having 4 to 12 carbon atoms; and (c) at least one aliphatic alcohol having 2 to 4 carbon atoms.

The invention claimed is: 
     
       1. An aqueous composition for topical application, comprising
 (a) at least one solid active agent having at 20° C. a solubility in water, 20° dH, of less than 5 g/L selected from the group consisting of minoxidil, erythromycin, dimetindene, betamethasone, ibuprofen, ketoprofen, diclofenac, metronidazole, acyclovir, imiquimod, docosanol and mixtures thereof; and 
 a solvent comprising a mixture of 
 (b) at least one 1,2-alkandiol having 4 to 12 carbon atoms; and 
 (c)at least one aliphatic alcohol having 2 to 4 carbon atoms. 
 
     
     
       2. The composition of  claim 1 , wherein the 1,2-alkandiol is selected from the group consisting of 1,2-butadiol, 1,2-pentandiol, 1,2-hexandiol, 1,2-heptandiol, 1,2-octandiol, 1,2-nonandiol, 1,2-decandiol, 1,2-undecandiol, 1,2,dodecandiol and mixtures thereof. 
     
     
       3. The composition of  claim 1 , wherein the aliphatic alcohol is selected from the group consisting of ethanol, n-propanol, isopropylalcohol, one of the isomeric butanols and mixtures thereof. 
     
     
       4. The composition of  claim 1 , wherein the 1,2-alkandiol is 1,2-pentandiol and the aliphatic alcohol is ethanol. 
     
     
       5. The composition of  claim 1 , comprising
 (a) about 1.0 to about 10.0% by weight of at least one solid active agent having at 20° C. a solubility in water (20° dH) of less than 5 g/L selected from the group consisting of minoxidil, erythromycin, dimetindene, betamethasone, ibuprofen, ketoprofen, diclofenac, metronidazole, acyclovir, imiquimod, docosanol and mixtures thereof, 
 (b) about 15 to about 50% by weight of at least 1,2-alkandiol having 4 to 12 carbon atoms; and; 
 (c) about 15 to about 25% by weight of at least one aliphatic alcohol having 2 to 4 carbon atoms, on condition that the amounts add with water to give 100% by weight. 
 
     
     
       6. A composition comprising
 (a) at least one solid active agent having at 20° C. a solubility in water (20° dH) of less than 5 g/L, selected from the group consisting of minoxidil, erythromycin, dimetindene, betamethasone, ibuprofen, ketoprofen, diclofenac, metronidazole, acyclovir, imiquimod, docosanol and mixtures thereof; 
 (b) at least one 1,2-alkandiol having 4 to 12 carbon atoms; and 
 (c) at least one aliphatic alcohol having 2 to 4 carbon atoms for the treatment of dermatologic diseases or pain. 
 
     
     
       7. The composition of  claim 6 , wherein the 1,2-alkandiol is selected from the group consisting of 1,2-butadiol, 1,2-pentandiol, 1,2-hexandiol, 1,2-heptandiol, 1,2-octandiol, 1,2-nonandiol, 1,2-decandiol, 1,2-undecandiol, 1,2,dodccandiol and mixtures thereof. 
     
     
       8. The composition of  claim 6 , wherein the aliphatic alcohol is selected from the group consisting of ethanol, n-propanol, isopropylalcohol, one of the isomeric butanols and mixtures thereof. 
     
     
       9. The composition of  claim 6 , wherein the composition is for topical or oral application. 
     
     
       10. The composition of  claim 6 , wherein the composition is a cream, a gel, a lotion, an ointment, a powder, a tablet or a capsule. 
     
     
       11. A method for improving solubility of a solid active agent in water, comprising dissolving the solid active agent in water in the presence of a mixture of solvent consisting of an 1,2-alkandiol having 4 to 12 carbon atoms and an aliphatic alcohol having 2 to 4 carbons, wherein the solid active agent having at 20° C. solubility in water, 20° dH, of less than 5 g/L is selected from group consisting of minoxidil, erythromycin, dimetindene, betamethasone, ibuprofen, ketoprofen, diclofenac, metronidazole, acyclovir, imiquimod, docosanol and mixtures thereof. 
     
     
       12. An aqueous composition for topical application, comprising
 (a) at least one solid agent having at 20° C. a solubility in water, 20° dH, of less than 5 g/L selected from the group consisting of minoxidil, ibuprofen, acyclovir, metronidazole, terbinafine, cyclopyroxolamine and mixtures thereof; and 
 a solvent comprising a mixture of 
 (b) 1,2-pentandiol; and 
 (c) ethanol.